US2010197689A1PendingUtilityA1

Novel processes for the preparation of piperazinyl and diazapanyl benzamide derivatives

Individually held — no corporate assignee on recordPriority: Oct 31, 2005Filed: Apr 19, 2010Published: Aug 5, 2010
Est. expiryOct 31, 2025(expired)· nominal 20-yr term from priority
A61P 43/00A61P 25/06A61P 25/08A61P 25/28A61P 17/04C07D 211/14C07D 295/182A61P 11/02C07D 295/192C07D 413/04A61P 11/06C07D 207/06C07D 295/18
38
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Claims

Abstract

The present invention is directed to novel processes for the preparation of substituted piperazinyl and diazepanyl benzamides, useful for the treatment of disorders and conditions mediated by the histamine receptor.

Claims

exact text as granted — not AI-modified
1 - 47 . (canceled) 
   
   
       48 . A crystalline succinate salt of (4-isopropyl-piperazin-1-yl)-(4-morpholin-4-ylmethyl-phenyl)-methanone. 
   
   
       49 . The salt of  claim 48 , wherein the succinate salt is a mono-succinate salt. 
   
   
       50 . A crystalline mono-succinate salt of (4-isopropyl-piperazin-1-yl)-(4-morpholin-4-ylmethyl-phenyl)-methanone comprising the following X-ray diffraction peaks: 
     
       
         
               
               
               
             
                   
                   
               
                   
                 Position [° 2θ] 
                 d-spacing [Å] 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 8.782 
                 10.0698 
               
                   
                 13.161 
                 6.7274 
               
                   
                 14.587 
                 6.0728 
               
                   
                 15.961 
                 5.5527 
               
                   
                 17.308 
                 5.1237 
               
                   
                 17.555 
                 5.0520 
               
                   
                 19.767 
                 4.4915 
               
                   
                 20.210 
                 4.3941 
               
                   
                 20.415 
                 4.3503 
               
                   
                 23.802 
                 3.7383 
               
                   
                 26.429 
                 3.3728 
               
                   
                   
               
           
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
              
              
              
              
              
              
             
          
         
       
     
   
   
       51 . A crystalline mono-succinate salt of (4-isopropyl-piperazin-1-yl)-(4-morpholin-4-ylmethyl-phenyl)-methanone comprising the following X-ray diffraction peaks: 
     
       
         
               
               
               
             
                   
                   
               
                   
                 Position [° 2θ] 
                 d-spacing [Å] 
               
                   
                   
               
                   
               
               
               
               
             
                   
                 8.782 
                 10.0698 
               
                   
                 13.161 
                 6.7274 
               
                   
                 17.555 
                 5.0520 
               
                   
                 23.802 
                 3.7383 
               
                   
                 26.429 
                 3.3728 
               
                   
                   
               
           
              
              
              
             
             
              
             
          
           
              
              
              
              
              
              
             
          
         
       
     
   
   
       52 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of  claim 49 . 
   
   
       53 . A pharmaceutical composition made by mixing a compound of  claim 49  and a pharmaceutically acceptable carrier. 
   
   
       54 . A process for making a pharmaceutical composition comprising mixing a compound of  claim 49  and a pharmaceutically acceptable carrier.

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